Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Matrices
Reexamination Certificate
2000-08-08
2001-05-22
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Matrices
C424S484000, C424S487000, C514S772400
Reexamination Certificate
active
06235314
ABSTRACT:
The present invention relates generally to a novel pharmaceutical composition matter comprising a non-steroidal anti-inflammatory drug (NSAID) in combination with a skeletal muscle relaxant, and more particularly to a topical ointment comprising a mixture of diazepam and an NSAID.
The oral ingestion of certain medications such as NSAIDs and diazepam (Valium®) is well known. The analgesic and anti-inflammatory properties of NSAIDs are also well known, as is the use of diazepam to treat symptoms of acute alcohol withdrawals, control epilepsy and to relieve muscle spasms as well as short term relief of mild to moderate anxiety. Further, studies have investigated the effectiveness of the transdermal delivery of diazepam and NSAIDs individually. It would appear that the effectiveness of the transdermal delivery depends largely on the vehicle for delivery of the drug, emulsions appearing more effective than creams.
SUMMARY OF THE INVENTION
It is therefore an object of the subject invention to provide a topical composition for relief of pain in an affected body part.
A further object to the subject invention is a combination of diazepam and diclofenac in a colorless transparent gel for application locally to an affected body part for the quick relief of pain.
These and other objects of the subject invention are obtained by the subject invention wherein there is provided a local skeletal muscle relaxant and a non-steroidal anti-inflammatory drug in a topical composition for topical application to a patient for relief of pain. More particularly and in its preferred form, the invention involves a combination of diazepam and diclofenac in a composition for topical application to the skin of a patient as a colorless transparent or translucent gel.
DETAILED DESCRIPTION OF THE INVENTION
The outstanding analgesic and anti-inflammatory properties of the non-steroidal anti inflammatory drugs compared to aspirin or acetaminophen have prompted the widespread acceptance and usage of these newer non-narcotic analgesics, as single entities, for the treatment and management of acute and chronic pain and inflammatory states, notably rheumatoid arthritis and osteoarthritis. However the utilization of these agents in topical skeletal muscle relaxant compositions has not heretofore been considered.
The non-steroidal anti-inflammatory drugs (NSAIDs) for use in the pharmaceutical compositions and methods of use of the present invention may be selected from any of the following categories:
(1) the propionic acid derivatives;
(2) the acetic acid derivatives;
(3) the fenamic acid derivatives;
(4) the biphenylcarboxylic and derivatives; and
(5) the oxicams.
Accordingly, the term “NSAID” as used herein is intended to mean any non-narcotic analgesic non-steroidal anti-inflammatory compound, including the pharmaceutically acceptable non-toxic salts thereof, falling within one of the five structural categories above but excluding aspirin, acetaminophen and phenacetin.
While some of the above-identified compounds are primarily used at the present time as anti-inflammatory agents and others are primarily used as analgesics, in fact all of the contemplated compounds have both analgesic and anti-inflammatory activity and can be used at appropriate dosage levels for either purpose in the compositions and methods of the present invention. The compounds in groups (1) to (4) typically contain a carboxylic acid function; however, those acids are sometimes administered in the form of their pharmaceutically acceptable salts, e.g. sodium salts.
The propionic acid derivatives for use herein include, but are not limited to, ibuprofen, naproxen benaxoprofen, naproxen sodium, flurbiprofen, fenoprofen, fenbufen, ketoprofen indoprofen, pirprofen, carprofen, oxaprozin, pranoprofen, microprofen, tioxaprofen, suprofen, alminoprofen, tiaprofenic acid, fluprofen and bucloxic acid. Structurally related propionic acid derivatives having similar analgesic and anti-inflammatory properties are also intended to be encompassed by this group. Representative members of the propionic acid group include ibuprofen, naproxen, flurbiprofen, fenbufen, fenoprofen, ibuprofen aluminum, ketoprofen, fluprofen and bucloxic acid.
Thus, “propionic acid derivatives” as defined herein are non-narcotic analgesics
on-steroidal anti-inflammatory drugs having a free —CH(CH
3
)COOH or —CH
2
CH
2
COOH group (which optionally can be in the form of pharmaceutically acceptable salt group, e.g. —CH(CH
3
) COO—Na+ or —CH
2
CH
2
COO—Na+), typically attached directly or via a carbonl function to a ring system, preferably to an aromatic ring system.
The acetic acid derivatives for use herein include, but are not limited to, indomethacin, sulindac, tolmetin, diclofenac, fenclofenac, alclofenac, ibufenac, isoxepac, furofenac, tiopinac, zidometacin, acemetacin, fentiazac, clidanac and oxepinac. Structurally related acetic acid derivatives having similar analgesic and anti-inflammatory properties are also intended to be encompassed by this group. Representative members of the acetic acid group include tolmetin, sulindac, indomethacin, diclofenac, alclofenac, fenclozic acid and ibufenac.
Thus, “acetic acid derivatives” as defined herein are non-narcotic analgesics
on-steroidal anti-inflammatory drugs having a free —CH
2
COOH group (which optionally can be in the form of a pharmaceutically acceptable salt group, e.g. —CH
2
COO—Na+), typically attached directly to a ring system, preferably to an aromatic or heteroaromatic ring system. The fenamic acid derivatives for use herein include, but are not limited to, mefenamic acid, meclofenamic acid, flufenamic acid, niflumic acid and tolfenamic acid. Structurally related fenamic acid derivatives having similar analgesic and anti-inflammatory properties are also intended to be encompassed by this group. Representative members of the fenamic acid group include mefenamic acid, meclofenamate sodium ( meclofenamic acid, sodium salt) and flufenamic acid. The biphenylcarboxylic acid derivatives for use herein include, but are not limited to, diflunisal and flufenisal. Structurally related biphenylcaboxylic acid derivatives having similar analgesic and anti-inflammatory properties are also intended to be encompassed by this group. Representative members of this group are diflunisal and flufenisal.
The term “skeletal muscle relaxant” as used herein is intended to mean diazepam, which has skeletal muscle relaxing properties. Diazepam acts directly on skeletal muscle and on the level of the central nervous system. Diazepam blocks impulses at the intemeurons of polysynaptic reflex arcs, mainly at the level of the spinal cord. This is demonstrated by the abolishment of the diminution of the flexor and crossed extensor reflexes which possess one or more interneurons between the sensory and motor fibers.
The newer non-steroidal anti-inflammatory drugs, which differ substantially in chemical structure from aspirin, acetaminophen and phenacetin, and which have significantly different biological profiles therefrom can be advantageously formulated into a novel composition together with diazepam and topically administered to mammals, especially to humans, to obtain more directed pain relief and lessened adverse side effects.
In accordance with the practices of the present invention, the NSAID/diazepam compositions may be administered in admixture with suitable pharmaceutical diluents, carrier or other excipients (collectively referred to as “carrier” materials) suitably selected with respect to the intended route of administration and conventional pharmaceutical practices. For instance, for topical administration in the form of a cream or ointment, the active drug components may be combined with any non-toxic pharmaceutically acceptable inert carrier such as a carbomer or other thickener and emulsifier.
A carbomer resin is an acrylic acid polymer, and more specifically comprises a water-swellable, but water-insoluble, fibrous, cross-linked carboxy-functional polymer. The polymer contains (a) a plurality of repeating units of which at lea
Bennett Rachel M.
Page Thurman K.
Welsh & Katz Ltd.
LandOfFree
Analgesic, anti-inflammatory and skeletal muscle relaxant... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Analgesic, anti-inflammatory and skeletal muscle relaxant..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Analgesic, anti-inflammatory and skeletal muscle relaxant... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2549401